KR20220157486A - 2-[(4-(6-[(4-시아노-2-플루오로벤질)옥시]피리딘-2-일)피페리딘-1-일)메틸]-1-[(2s)-옥세탄-2-일메틸]-1h-벤즈이미다졸-6-카르복실산 또는 그의 제약상 염을 사용한 제2형 당뇨병 또는 비만 또는 과체중의 치료 - Google Patents

2-[(4-(6-[(4-시아노-2-플루오로벤질)옥시]피리딘-2-일)피페리딘-1-일)메틸]-1-[(2s)-옥세탄-2-일메틸]-1h-벤즈이미다졸-6-카르복실산 또는 그의 제약상 염을 사용한 제2형 당뇨병 또는 비만 또는 과체중의 치료 Download PDF

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KR20220157486A
KR20220157486A KR1020227036905A KR20227036905A KR20220157486A KR 20220157486 A KR20220157486 A KR 20220157486A KR 1020227036905 A KR1020227036905 A KR 1020227036905A KR 20227036905 A KR20227036905 A KR 20227036905A KR 20220157486 A KR20220157486 A KR 20220157486A
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pharmaceutical composition
compound
pyridin
oxy
fluorobenzyl
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English (en)
Korean (ko)
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카이 테크 리
스웨타 만테나
아디티 라오 사세나
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화이자 인코포레이티드
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
KR1020227036905A 2020-03-27 2021-03-24 2-[(4-(6-[(4-시아노-2-플루오로벤질)옥시]피리딘-2-일)피페리딘-1-일)메틸]-1-[(2s)-옥세탄-2-일메틸]-1h-벤즈이미다졸-6-카르복실산 또는 그의 제약상 염을 사용한 제2형 당뇨병 또는 비만 또는 과체중의 치료 Withdrawn KR20220157486A (ko)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US202063000787P 2020-03-27 2020-03-27
US63/000,787 2020-03-27
US202063126113P 2020-12-16 2020-12-16
US63/126,113 2020-12-16
US202163135870P 2021-01-11 2021-01-11
US63/135,870 2021-01-11
PCT/IB2021/052430 WO2021191812A1 (en) 2020-03-27 2021-03-24 Treatment of type 2 diabetes or obesity or overweight with 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl} piperidin-1-yl)methyl]-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid or a pharmaceutically salt thereof

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KR20220157486A true KR20220157486A (ko) 2022-11-29

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KR1020227036905A Withdrawn KR20220157486A (ko) 2020-03-27 2021-03-24 2-[(4-(6-[(4-시아노-2-플루오로벤질)옥시]피리딘-2-일)피페리딘-1-일)메틸]-1-[(2s)-옥세탄-2-일메틸]-1h-벤즈이미다졸-6-카르복실산 또는 그의 제약상 염을 사용한 제2형 당뇨병 또는 비만 또는 과체중의 치료

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US (1) US20230201185A1 (enExample)
EP (2) EP4537816A3 (enExample)
JP (2) JP2021155415A (enExample)
KR (1) KR20220157486A (enExample)
CN (1) CN115348863A (enExample)
AU (1) AU2021244918A1 (enExample)
BR (1) BR112022017578A2 (enExample)
CA (1) CA3176569A1 (enExample)
ES (1) ES3031577T3 (enExample)
IL (1) IL296694A (enExample)
MX (1) MX2022010811A (enExample)
TW (1) TWI823072B (enExample)
WO (1) WO2021191812A1 (enExample)

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AU2020256647B2 (en) 2019-04-12 2025-07-31 Qilu Regor Therapeutics Inc. GLP-1R agonists and uses thereof
CR20220178A (es) 2019-10-25 2022-06-15 Gilead Sciences Inc Compuestos moduladores de glp-1r
SI4097097T1 (sl) 2020-01-29 2025-04-30 Gilead Sciences, Inc. Spojine, ki modulirajo glp-1r
EP4247804A1 (en) 2020-11-20 2023-09-27 Gilead Sciences, Inc. Polyheterocyclic glp-1 r modulating compounds
US12180197B2 (en) 2021-03-11 2024-12-31 Gilead Sciences, Inc. GLP-1R modulating compounds
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US12024507B2 (en) 2021-10-25 2024-07-02 Terns Pharmaceuticals, Inc. Compounds as GLP-1R agonists
CA3246495A1 (en) * 2022-03-25 2023-09-28 Ildong Pharmaceutical Co., Ltd. NEW GLP-1 RECEPTOR AGONIST COMPOUND SALT, ITS PREPARATION PROCESS AND PHARMACEUTICAL COMPOSITION INCLUDING IT
KR20250036254A (ko) * 2022-07-22 2025-03-13 화이자 인코포레이티드 2-[(4-｛6-[(4-시아노-2-플루오로벤질)옥시]피리딘-2-일}피페리딘-1-일｝메틸]-1-[(2s)-옥세탄-2-일메틸]-1h-벤즈이미다졸-6-카복실산,1,3-다이하이드록시-2-(하이드록시메틸)프로판-2-아민 염의 제조를 위한 방법 및 중간체
PE20252787A1 (es) 2023-04-07 2025-12-22 Terns Pharmaceuticals Inc Combinacion que comprende un agonista de thr-beta y un agonista de glp-1r para su uso en el tratamiento de un trastorno hepatico o una enfermedad cardiometabolica
CN116675680B (zh) * 2023-08-02 2023-10-20 药康众拓(北京)医药科技有限公司 一种氘代化合物及其制备方法、药物和应用
EP4777197A2 (en) 2023-09-14 2026-07-22 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof
WO2025099561A1 (en) 2023-11-07 2025-05-15 Pfizer Inc. Oral controlled-release matrix formulations of 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid or a pharmaceutically salt thereof
WO2025109387A1 (en) 2023-11-24 2025-05-30 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof
WO2025224648A1 (en) * 2024-04-26 2025-10-30 Pfizer Inc. Oral compositions/formulations of 2-({4-[(2s)-2-(4-chloro-2-fluorophenyl)-2-methyl-1,3-benzodioxol-4-yl]piperidin-1-yl}methyl)-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid or a pharmaceutically salt thereof
TW202612693A (zh) * 2024-06-05 2026-04-01 大陸商杭州中美華東製藥有限公司 Glp-1受體激動劑的口服藥物組合物及其製備方法

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ES3031577T3 (en) 2025-07-09
BR112022017578A2 (pt) 2022-10-18
EP4537816A2 (en) 2025-04-16
EP4125896B1 (en) 2025-05-07
TWI823072B (zh) 2023-11-21
AU2021244918A1 (en) 2022-09-29
EP4537816A3 (en) 2025-06-25
IL296694A (en) 2022-11-01
US20230201185A1 (en) 2023-06-29
WO2021191812A1 (en) 2021-09-30
CN115348863A (zh) 2022-11-15
MX2022010811A (es) 2022-09-27
JP2021155415A (ja) 2021-10-07
JP2025118943A (ja) 2025-08-13
EP4125896A1 (en) 2023-02-08
CA3176569A1 (en) 2021-09-30
TW202202139A (zh) 2022-01-16

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